RNA-BINDING EFFICACY OF N-PHENYLBENZOHYDROXAMIC ACID: AN INVITRO AND INSILICO APPROACH

被引:8
|
作者
Khilari, Rubi [1 ]
Thakur, Yamini [1 ]
Pardhi, Manish [1 ]
Pande, Rama [1 ]
机构
[1] Pt Ravishankar Shukla Univ, Sch Studies Chem, Raipur, Chhattisgarh, India
来源
关键词
Hydroxamic acid; PBHA; RNA; binding; fluorescence; viscosity; intercalation; SUBEROYLANILIDE HYDROXAMIC ACID; PLANT ALKALOID PALMATINE; SMALL MOLECULES; ARYLHYDROXAMIC ACIDS; PROTEIN INTERACTIONS; DNA; BERBERINE; ETHIDIUM; POLY(A); MICRORNAS;
D O I
10.1080/15257770.2014.1001073
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
RNA has attracted recent attention for its key role in gene expression and hence targeting by small molecules for therapeutic intervention. This study is aimed to elucidate the specificity of RNA binding affinity of parent compound of N-arylhydroxamic acids series, N-phenylbenzohydroxamic acid trivially named as PBHA,C6H5NOH.C6H5C O. The binding behavior was examined by various biophysical methods such as absorption, fluorescence, and viscosity measurements. Molecular docking was also done. The value of affinity constant and overall binding constant was calculated 5.79 +/- 0.03 x 10(4) M-1 and K' = 1.09 +/- 0.03 x 10(5) M-1, respectively. The Stern-Volmer constant K-sv obtained was 2.28 +/- 0.04 x 10(4) M-1. The compound (PBHA) shows a concentration-based enhancement of fluorescence intensity with increasing RNA concentration. Fluorescence quenching of PBHA-RNA complex in presence of K-4 [Fe(CN)(6)] was also observed. Viscometric studies complimented the UV results where a continuous increase in relative viscosity of the RNA solution was observed with added optimal PBHA concentration. All the experimental evidences indicate that PBHA can strongly bind to RNA through an intercalative mode.
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页码:332 / 347
页数:16
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